Effect of Kenpaullone, a Specific Inhibitor of GSK3β, on Melanin Synthesis in B16 Melanoma and Human Melanocytes

Abstract

Effects of Kenpaullone, a specific inhibitor of GSK3, on melanin synthesis in B16 melanoma cells and human melanocytes were investigated. Kenpaullone showed a melanogenesis stimulation activity in a concentrationdependent manner in murine B16 melanoma cells and human melanocytes without any significant effects on cell proliferation. Tyrosinase activity was increased 48 h after treatment of B16 cells with Kenpaullone. The protein expression level of tyrosinase was dose-dependently enhanced after the treatment with Kenpaullone. At the same time, the expression level of tyrosinase mRNA was also increased after addition of Kenpaullone. The stimulatory effect of Kenpaullone mainly resulted from increased expression of tyrosinase. These findings suggest that the application of GSK3 inhibitors may be a potential therapeutic agent for the treatment of hypopigmentation disorder.